US2006223837A1PendingUtilityA1
Biaryl derived amide modulators of vanilloid VR1 receptor
Est. expiryMar 24, 2025(expired)· nominal 20-yr term from priority
C07D 235/06C07D 233/64C07D 213/53C07C 237/42C07D 401/12C07D 291/04C07D 333/24C07D 233/68C07D 271/06C07C 233/29C07C 233/55C07D 401/04C07D 213/75A61P 29/00
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Claims
Abstract
The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
Claims
exact text as granted — not AI-modified1 . A compound of Formula (I):
wherein:
A1 is phenyl, naphthalenyl, pyridinyl, or thienyl;
R 1 is independently hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, trifluoromethylsulfonyl, trifluoromethylsulfinyl, fluorinated alkanyl, and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl, and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanylsulfinyl optionally substituted with one or more substituents independently selected from the group consisting of halogen and C 1-8 alkanyloxy; C 1-8 alkanylsulfonyl optionally substituted with one or more substituents independently selected from the group consisting of halogen and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; N—C 1-8 alkanyl-N—C 3-8 cycloalkanylamino, cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; formyl; aminosulfonyl; C 1-8 alkanylaminosulfonyl; di(C 1-8 )alkanylaminosulfonyl; or cyano;
p is 0, 1 or 2;
L is C 2-8 alkandiyl, C 2-8 alkendiyl, or C 2-8 alkyndiyl and L is optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, C 1-8 alkanyloxy, halogen, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
X is O or S;
A2 is selected from the group consisting of phenyl, thien-2-yl, naphthalenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolinyl, and isoquinolinyl;
R 2 is independently selected from the group consisting of C 1-8 alkanyl, C 1-8 alkanyloxy, hydroxy(C 1-8 )alkanyl, fluorinated C 1-8 alkanyl, hydroxyl, halogen, carboxy, C 1-8 alkanyloxycarbonyl, and aminocarbonyl;
q is 0, 1, or 2;
A3 is selected from the group consisting of phenyl, thienyl, naphthalenyl, pyridinyl, pyrimidinyl, pyrazinyl, imidazolyl, oxazolyl, 4,5-dihydro-oxazolyl, pyrazolyl, dihydro-pyrazolyl, thiazolyl, thiadiazolyl, triazolyl, tetrazolyl, quinolinyl, isoquinolinyl, oxathiadiazolyl, benzimidazolyl, tetrahydrobenzimidazolyl, tetrahydroindazolyl, oxathiadiazolyl 2-oxide, oxadiazolyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, and indolyl;
such that when A3 is tetrahydrobenzimidazolyl, tetrahydroindazolyl, oxathiadiazolyl 2-oxide, tetrahydroisoquinolinyl, or tetrahyd roquinolinyl, then r is 0;
R 3 is independently selected from the group consisting of hydroxy; halogen; C 1-8 alkanyl; hydroxy(C 1-8 )alkanyl; C 1-8 alkanyloxy optionally substituted with amino, C 1-8 alkanylamino, or C 1-8 dialkanylamino; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; aminosulfonyl; carboxy; C 1-8 alkanylsulfonylamino; aminocarbonyl; C 1-8 alkanyloxycarbonyl; C 1-4 alkanyloxycarbonylamino; C 1-8 alkanylaminocarbonyl; C 1-8 alkanylcarbonylamino; diC 1-8 alkanylaminocarbonyl; oxo when A3 is dihydro-pyrazolyl; and formyl; and wherein the C 1-8 alkanyl group of any C 1-8 alkanylamino and C 1-8 dialkanylamino containing substituent of R 3 is optionally substituted with hydroxy;
r is 0, 1, or 2;
R 4 is hydrogen or C 1-8 alkyl;
provided that a compound of Formula 1 is other than
a compound wherein p is 1, R 1 is 4-trifluoromethylsulfonyl, A1 is phenyl, L is trans —CH═CH—, X is O, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is imidazol-1-yl, r is 2, R 3 is 4,5-dichloro, and R 4 is hydrogen;
a compound wherein p is 1, R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, X is O, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is pyrazol-1-yl, r is 2, R 3 is 3,5-dimethyl, and R 4 is hydrogen;
a compound wherein p is 1, R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, X is O, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is imidazol-1-yl, r is 1, R 3 is 4-carboxy, and R 4 is hydrogen; and
enantiomers, diastereomers, tautomers, solvates, and
pharmaceutically acceptable salts thereof.
2 . A compound of Formula (I)
wherein:
A1 is phenyl, naphthalenyl, or thienyl;
R 1 is independently hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl, and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; formyl; aminosulfonyl; C 1-8 alkanylaminosulfonyl; di(C 1-8 )alkanylaminosulfonyl; or cyano;
p is 0, 1 or 2;
L is C 2-8 alkandiyl, C 2-8 alkendiyl, or C 2-8 alkyndiyl and L is optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, C 1-8 alkanyloxy, halogen, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
X is O or S;
A2 is selected from the group consisting of phenyl, thien-2-yl, naphthalenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolinyl, and isoquinolinyl;
R 2 is independently selected from the group consisting of C 1-8 alkanyl, C 1-8 alkanyloxy, hydroxy(C 1-8 )alkanyl, fluorinated C 1-8 alkanyl, hydroxyl, halogen, carboxy, C 1-8 alkanyloxycarbonyl, and aminocarbonyl;
q is 0, 1, or 2;
A3 is selected from the group consisting of phenyl, thienyl, naphthalenyl, pyridinyl, pyrimidinyl, pyrazinyl, imidazolyl, oxazolyl, 4,5-dihydro-oxazolyl, pyrazolyl, dihydro-pyrazolyl, thiazolyl, thiadiazolyl, triazolyl, tetrazolyl, quinolinyl, isoquinolinyl, and indolyl;
R 3 is independently selected from the group consisting of hydroxy; halogen; C 1-8 alkanyl; hydroxy(C 1-8 )alkanyl; C 1-8 alkanyloxy optionally substituted with amino, C 1-8 alkanylamino, or C 1-8 dialkanylamino; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; aminosulfonyl; carboxy; C 1-8 alkanylsulfonylamino; aminocarbonyl; C 1-8 alkanyloxycarbonyl; C 1-4 alkanyloxycarbonylamino; C 1-8 alkanylaminocarbonyl; C 1-8 alkanylcarbonylamino; diC 1-8 alkanylaminocarbonyl; oxo when A3 is dihydro-pyrazolyl; and formyl; and wherein the C 1-8 alkanyl group of any C 1-8 alkanylamino and C 1-8 dialkanylamino containing substituent of R 3 is optionally substituted with hydroxy;
r is 0, 1, or 2;
R 4 is hydrogen or C 1-8 alkyl; and enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
3 . The compound according to claim 1 wherein A1 is phenyl, pyridinyl, or thienyl.
4 . The compound according to claim 1 wherein A1 is phenyl, pyridinyl, or thienyl, and p is 1 or 2.
5 . The compound according to claim 1 or 2 wherein A1 is phenyl or thienyl.
6 . The compound according to claim 1 or 2 wherein A1 is phenyl or thienyl, and p is 1 or 2.
7 . The compound according to claim 1 or 2 wherein A1 is phenyl substituted at the 4-position with R 1 , or thiophen-2-yl substituted at the 5-position with R 1 .
8 . The compound according to claim 1 wherein R 1 is independently C 1-6 alkanyl, fluorinated C 1-6 alkanyl; C 1-8 alkanylsulfonyl substituted with one to three fluoro substituents; C 1-8 alkanylthio substituted with one to three fluoro substituents; C 1-8 alkanylsulfinyl substituted with one to three fluoro substituents; chloro; fluoro; or N—C 1-4 alkanyl-N-cyclohexylamino.
9 . The compound according to claim 1 wherein R 1 is C 1-4 alkanyl; fluorinated C 1-4 alkanyl; trifluoromethylsulfonyl; trifluoromethylthio; trifluoromethylsulfinyl; chloro; or N-methyl-N-cyclohexylamino.
10 . The compound according to claim 1 wherein R 1 is independently t-butyl, trifluoromethyl, trifluoromethylsulfonyl, or trifluoromethylthio.
11 . The compound according to claim 1 or 2 wherein R 1 is independently C 1-6 alkanyl or fluorinated C 1-6 alkanyl.
12 . The compound according to claim 1 or 2 wherein R 1 is independently C 1-4 alkanyl or fluorinated C 1-4 alkanyl.
13 . The compound according to claim 1 or 2 wherein R 1 is independently t-butyl or trifluoromethyl.
14 . The compound according to claim 1 or 2 wherein p is 1 or 2.
15 . The compound according to claim 1 or 2 wherein p is 1.
16 . The compound according to claim 1 or 2 wherein L is C 2-8 alkandiyl, C 2-8 alkendiyl, or C 2-8 alkyndiyl and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl, and phenyl.
17 . The compound according to claim 1 or 2 wherein L is C 2-4 alkandiyl or C 2-4 alkendiyl, and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl, and phenyl.
18 . The compound according to claim 1 or 2 wherein L is —CH 2 CH 2 — or —CH═CH—.
19 . The compound according to claim 1 or 2 wherein X is O or S.
20 . The compound according to claim 1 or 2 wherein X is O.
21 . The compound according to claim 1 or 2 wherein q is 0, 1, or 2, and A2 is selected from the group consisting of phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolinyl, and isoquinolinyl.
22 . The compound according to claim 1 or 2 wherein q is 0, 1, or 2, and A2 is selected from the group consisting of phenyl, pyridinyl, and isoquinolinyl.
23 . The compound according to claim 1 or 2 wherein q is 0, 1, or 2 and A2 is selected from the group consisting of phenyl, pyridin-3-yl, and isoquinolin-5-yl.
24 . The compound according to claim 1 or 2 wherein R 2 is independently selected from the group consisting of C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, fluorinated C 1-4 alkanyl, and fluoro.
25 . The compound according to claim 1 or 2 wherein R 2 is independently selected from the group consisting of methyl, hydroxymethyl, and fluoro.
26 . The compound according to claim 1 or 2 wherein q is 1 or 2.
27 . The compound according to claim 1 wherein r is 1 or 2 and A3 is selected from the group consisting of phenyl, thienyl, pyridinyl, pyrimidinyl, and imidazolyl.
28 . The compound according to claim 1 wherein r is 1 or 2 and when A2 is phenyl, A3 is 4-phenyl, 3-phenyl, 2-pyridin-4-yl, 2-pyridin-2-yl, 3-pyridin-4-yl, 2-pyridin-3-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl, 3-pyrimidin-2-yl or 4-imidazol-1-yl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, 6-pyridin-4-yl, or 6-imidazol-1-yl.
29 . The compound according to claim 1 wherein r is 1 or 2 and when A2 is phenyl, A3 is 4-phenyl, 3-phenyl, 2-pyridin-2-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl, 3-pyrimidin-2-yl, or 4-imidazol-1-yl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, 6-pyridin-4-yl, or 6-imidazol-1-yl.
30 . The compound according to claim 1 or 2 wherein r is 1 or 2 and A3 is selected from the group consisting of phenyl, pyridinyl, and pyrimidinyl.
31 . The compound according to claim 1 or 2 wherein r is 1 or 2 and when A2 is phenyl, A3 is 4-phenyl, 3-phenyl, 2-pyridin-4-yl, 2-pyridin-2-yl, 3-pyridin-4-yl, 2-pyridin-3-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl or 3-pyrimidin-2-yl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, or 6-pyridin-4-yl.
32 . The compound according to claim 1 or 2 wherein r is 1 or 2 and when A2 is phenyl, A3 is 4-phenyl, 3-phenyl, 2-pyridin-2-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl or 3-pyrimidin-2-yl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, or 6-pyridin-4-yl.
33 . The compound according to claim 1 or 2 wherein R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, C 1-4 alkanyloxy optionally substituted with amino, C 1-4 alkanylamino, or C 1-4 dialkanylamino, fluorinated alkanyloxy, fluorinated alkanyl, amino, C 1-4 alkanylamino, C 1-4 dialkanylamino, C 3-8 cycloalkanylamino, cyano, aminosulfonyl, C 1-4 alkanylsuIfonylamino, C 1-4 alkanyloxycarbonyl, C 1-4 alkanyloxycarbonylamino, aminocarbonyl, C 1-4 alkanylaminocarbonyl, C 1-4 alkanylcarbonylamino, diC 1-4 alkanylaminocarbonyl, and formyl; and wherein C 1-4 alkanyl in any of the foregoing C 1-4 alkanylamino and C 1-4 dialkanylamino containing substituents of R 3 is optionally substituted with hydroxy.
34 . The compound according to claim 1 wherein R 3 is independently selected from the group consisting of hydroxyl, fluoro, chloro, methyl, hydroxymethyl, C 1-3 alkanyloxy optionally substituted with amino, methylamino, or dimethylamino, trifluoromethoxy, trifluoromethyl, methylsulfonylamino, t-butoxycarbonylamino, aminocarbonyl, and methylcarbonylamino.
35 . The compound according to claim 1 wherein R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, methyl, hydroxymethyl, 2-aminoethoxy, methylsulfonylamino, and methylcarbonylamino.
36 . The compound according to claim 1 or 2 wherein R 3 is independently selected from the group consisting of hydroxyl, fluoro, methyl, hydroxymethyl, C 1-3 alkanyloxy optionally substituted with amino, methylamino, or dimethylamino, trifluoromethoxy, trifluoromethyl, methylsulfonylamino, t-butoxycarbonylamino, aminocarbonyl, and methylcarbonylamino.
37 . The compound according to claim 1 or 2 wherein R 3 is independently selected from the group consisting of hydroxy, fluoro, methyl, hydroxymethyl, 2-aminoethoxy, methylsulfonylamino, and methylcarbonylamino.
38 . The compound according to claim 1 or 2 wherein r is 1 or 2.
39 . The compound according to claim 1 or 2 wherein r is 1.
40 . The compound according to claim 1 or 2 wherein R 4 is hydrogen or C 1-4 alkyl.
41 . The compound according to claim 1 wherein R 4 is hydrogen.
42 . A compound of Formula (I)
wherein:
A1 is phenyl, pyridinyl, or thienyl;
R 1 independently is C 1-6 alkanyl; fluorinated C 1-6 alkanyl; C 1-8 alkanylsulfonyl substituted with one to three fluoro substituents; C 1-8 alkanylthio substituted with one to three fluoro substituents; C 1-8 alkanylsulfinyl substituted with one to three fluoro substituents; chloro; fluoro; or N—C 1-4 alkanyl-N-cyclohexylamino;
p is 1 or 2;
L is C 2-8 alkandiyl, C 2-8 alkendiyl, or C 2-8 alkyndiyl and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl and phenyl;
X is O or S;
A2 is selected from the group consisting of phenyl, thienyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolinyl, and isoquinolinyl;
R 2 is independently selected from the group consisting of C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, fluorinated C 1-4 alkanyl, and fluoro;
q is 1 or 2;
A3 is selected from the group consisting of phenyl, thienyl, pyridinyl, pyrimidinyl, and imidazolyl;
R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, C 1-4 alkanyloxy optionally substituted with amino, C 1-4 alkanylamino, or C 1-4 dialkanylamino, fluorinated alkanyloxy, fluorinated alkanyl, amino, C 1-4 alkanylamino, C 1-4 dialkanylamino, C 3-8 cycloalkanylamino, cyano, aminosulfonyl, C 1-4 alkanylsulfonylamino, C 1-4 alkanyloxycarbonyl, C 1-4 alkanyloxycarbonylamino, aminocarbonyl, C 1-4 alkanylaminocarbonyl, C 1-4 alkanylcarbonylamino, diC 1-4 alkanylaminocarbonyl, and formyl, and wherein C 1-4 alkanyl in any of the foregoing C 1-4 alkanylamino and C 1-4 dialkanylamino containing substituent of R 3 is optionally substituted with hydroxy;
R 4 is hydrogen or C 1-4 alkyl,
provided that a compound of Formula 1 is other than
a compound wherein p is 1, R 1 is 4-trifluoromethylsulfonyl, A1 is phenyl, L is trans —CH═CH—, X is O, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is imidazol-1-yl, r is 2, R 3 is 4,5-dichloro, and R 4 is hydrogen; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
43 . A compound of Formula 1 wherein:
A1 is phenyl, pyridinyl, or thienyl; R 1 is independently C 1-4 alkanyl; fluorinated C 1-4 alkanyl; trifluoromethylsulfonyl; trifluoromethylthio; trifluoromethylsulfinyl; chloro; or N-methyl-N-cyclohexylamino; p is 1; L is C 2-4 alkandiyl or C 2-4 alkendiyl, and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl and phenyl; X is O; A2 is selected from the group consisting of phenyl, thienyl, pyridinyl, and isoquinolinyl; R 2 is independently selected from the group consisting of methyl, hydroxymethyl, trifluoromethyl, and fluoro; q is 0, 1, or 2; A3 is 4-phenyl, 3-phenyl, 2-pyridin-4-yl, 2-pyridin-2-yl, 3-pyridin-4-yl, 2-pyridin-3-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl, 3-pyrimidin-2-yl or 4-imidazol-1-yl when A2 is phenyl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, 6-pyridin-4-yl, or 6-imidazol-1-yl; R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, methyl, hydroxymethyl, C 1-3 alkanyloxy optionally substituted with amino, methylamino, or dimethylamino, trifluoromethoxy, trifluoromethyl, methylsulfonylamino, t-butoxycarbonylamino, aminocarbonyl, and methylcarbonylamino; r is 1; R 4 is hydrogen, and enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
44 . A compound of Formula (I)
wherein:
A1 is phenyl or thienyl;
R 1 independently is C 1-6 alkanyl or fluorinated C 1-6 alkanyl;
p is 1 or 2;
L is C 2-8 alkandiyl, C 2-8 alkendiyl, or C 2-8 alkyndiyl and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl and phenyl;
X is O or S;
A2 is selected from the group consisting of phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolinyl, and isoquinolinyl;
R 2 is independently selected from the group consisting of C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, fluorinated C 1-4 alkanyl, and fluoro;
q is 1 or 2;
A3 is selected from the group consisting of phenyl, pyridinyl, and pyrimidinyl;
R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, C 1-4 alkanyl, hydroxy(C 1-4 )alkanyl, C 1-4 alkanyloxy optionally substituted with amino, C 1-4 alkanylamino, or C 1-4 dialkanylamino, fluorinated alkanyloxy, fluorinated alkanyl, amino, C 1-4 alkanylamino, C 1-4 dialkanylamino, C 3-8 cycloalkanylamino, cyano, aminosulfonyl, C 1-4 alkanylsuIfonylamino, C 1-4 alkanyloxycarbonyl, C 1-4 alkanyloxycarbonylamino, aminocarbonyl, C 1-4 alkanylaminocarbonyl, C 1-4 alkanylcarbonylamino, diC 1-4 alkanylaminocarbonyl, and formyl, and wherein C 1-4 alkanyl in any of the foregoing C 1-4 alkanylamino and C 1-4 dialkanylamino containing substituent of R 3 is optionally substituted with hydroxy;
R 4 is hydrogen or C 1-4 alkyl, and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
45 . A compound of Formula 1 wherein:
A1 is phenyl or thienyl; R 1 is independently C 1-4 alkanyl or fluorinated C 1-4 alkanyl; p is 1; L is C 2-4 alkandiyl or C 2-4 alkendiyl, and L is optionally substituted with a substituent selected from the group consisting of C 1-4 alkanyl, C 3-8 cycloalkanyl and phenyl; X is O; A2 is selected from the group consisting of phenyl, pyridinyl, and isoquinolinyl; R 2 is independently selected from the group consisting of methyl, hydroxymethyl, and fluoro; q is 0, 1, or 2; A3 is 4-phenyl, 3-phenyl, 2-pyridin-4-yl, 2-pyridin-2-yl, 3-pyridin-4-yl, 2-pyridin-3-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl or3-pyrimidin-2-yl when A2 is phenyl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, or 6-pyridin-4-yl; R 3 is independently selected from the group consisting of hydroxy, fluoro, methyl, hydroxymethyl, C 1-3 alkanyloxy optionally substituted with amino, methylamino, or dimethylamino, trifluoromethoxy, trifluoromethyl, methylsulfonylamino, t-butoxycarbonylamino, aminocarbonyl, and methylcarbonylamino; r is 1; R 4 is hydrogen, and enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
46 . A compound of Formula Ia:
wherein:
A1 is phenyl substituted at the 4-position with R 1 , or thiophen-2-yl substituted at the 5-position with R 1 ;
R 1 is independently t-butyl or trifluoromethyl,
L is —CH 2 CH 2 — or —CH═CH—;
A2 is selected from the group consisting of phenyl, pyridin-3-yl, and isoquinolin-5-yl optionally substituted with R 2 ;
R 2 is independently selected from the group consisting of hydrogen, methyl, hydroxymethyl, and fluoro;
q is 0, 1, or 2;
A3 is 4-phenyl, 3-phenyl, 2-pyridin-2-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl or 3-pyrimidin-2-yl when A2 is phenyl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, or 6-pyridin-4-yl;
R 3 is independently selected from the group consisting of hydroxy, fluoro, methyl, hydroxymethyl, 2-aminoethoxy, methylsulfonylamino, and methylcarbonylamino, and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
47 . A compound of Formula Ia:
wherein:
A1 is phenyl substituted at the 4-position with R 1 , or thiophen-2-yl substituted at the 5-position with R 1 ;
R 1 is independently t-butyl, trifluoromethyl, trifluoromethylsulfonyl, or trifluoromethylthio;
L is —CH 2 CH 2 — or —CH═CH—;
A2 is selected from the group consisting of phenyl, pyridin-3-yl, and isoquinolin-5-yl optionally substituted with R 2 ;
R 2 is independently selected from the group consisting of methyl, hydroxymethyl, trifluoromethyl, and fluoro;
q is 0, 1, or 2;
A3 is 4-phenyl, 3-phenyl, 2-pyridin-2-yl, 4-pyridin-4-yl, 4-pyridin-3-yl, 4-pyridin-2-yl, 4-pyrimidin-5-yl, 3-pyrimidin-2-yl or 4-imidazol-1-yl when A2 is phenyl; and when A2 is isoquinolin-5-yl, A3 is 8-pyridin-4-yl or 8-phenyl; and when A2 is pyridin-3-yl, A3 is 6-phenyl, 6-pyridin-3-yl, 6-pyridin-2-yl, 6-pyridin-4-yl, or 6-imidazol-1-yl;
R 3 is independently selected from the group consisting of hydroxy, fluoro, chloro, methyl, hydroxymethyl, 2-aminoethoxy, methylsulfonylamino, and methylcarbonylamino,
provided that a compound of Formula 1 is other than a compound wherein p is 1, R 1 is 4-trifluoromethylsulfonyl, A1 is phenyl, L is trans —CH═CH—, X is O, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is imidazol-1-yl, r is 2, R 3 is 4,5-dichloro, and R 4 is hydrogens
and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
48 . A compound of Formula Ia
selected from the group consisting of:
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0; R 2 is absent; A3 is 2-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-nitro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-trifluoromethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-chloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-fluoro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-amino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L-is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-cyano;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-trifluoromethoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methoxycarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-carboxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylsulfonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-t-butoxycarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-t-butoxycarbonylaminomethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminomethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-ureido;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-(2-amino-ethoxy);
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-(2-hydroxy-ethylamino);
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R, is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-methylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrimidin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrimidin-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 1, and R 3 is 6-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyrimidin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R, is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyrimidin-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-3-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1 H-indol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1H-indol-6-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is-0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrimidin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-3-yl, r is 0, and R 3 absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen- -yl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is-phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent,
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-2-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-4-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-5-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-oxazol-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(4,5-dihydro-oxazol-5-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is ′—(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-thiazol-4-yl, r is 1, and R 3 is 2-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrazol-1-yl, r is 2, and R 3 is 3,5-dimethyl
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-thiadiazol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(1,2,4-triazol-1-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1 H-tetrazol-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-3-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(2,4-dihydro-pyrazol-2-yl), r is 2, and R 3 is 3-oxo, 5-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulphonyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-phenyl, and r is 1, R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulphonyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, and r is 0, R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulphonyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-pyridin-4-yl, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulphanyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and. R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-chloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-chloro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-chloro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-N-cyclohexyl-N-methylamino, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 4-chloro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethylsulfonyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethylsulfonyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-trifluoromethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-N-cyclohexyl-N-methylamino, A1 is phenyl, L is trans —CH═CH—, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-chloro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-fluoro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulfinyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-(2-oxo-2,3-dihydro-2λ4-[1,2,3,5]oxathiadiazol-4-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-cyano;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, and r is 2, R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is hydrogen, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-benzoimidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-pyridin-4-yl, r is 1, and R 3 is 2-fluoro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-trifluoromethyl, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 3,4-difluoro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 3,4-difluoro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-pyridin-3-yl, r is 1, and R 3 is 2-fluoro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-nitro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-(1,2,4-oxadiazol-3-yl), r is 1, and R 3 is 5-trifluoromethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-(1,2,4-oxadiazol-3-yl), r is 1, and R 3 is 5-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 2-methyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 2-isopropyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-indol-1-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-(4,5,6,7-tetrahydro-benzoimidazol-1-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methoxycarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulfinyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylsulfinyl, A1 is phenyl, L is trans —CH═CH—, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethylthio, A1 is phenyl, L is trans —CH═CH—, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is trans —CH═CH—, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is trans —CH═CH—, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 1, and R 3 is 4-methyl;
a compound of Formula (Ia) wherein R 1 is 5-trifluoromethyl, A1 is pyridin-2-yl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro;
a compound of Formula (Ia) wherein R 1 is 4-fluoro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-trifluoromethyl, A3 is 4-imidazol-1-yl, r is 0, and R 3 is absent;
and
a compound of Formula (Ia) wherein R 1 is 4-fluoro, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-imidazol-1-yl, r is 2, and R 3 is 4,5-dichloro.
49 . A compound of Formula Ia
selected from the group consisting of:
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0; R 2 is absent; A3 is 2-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-nitro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-trifluoromethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-chloro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-fluoro;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-amino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-cyano;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-trifluoromethoxy,
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methoxycarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-carboxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-dimethylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylsulfonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-t-butoxycarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-t-butoxycarbonylaminomethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminomethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-ureido;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-(2-amino-ethoxy);
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-(2-hydroxy-ethylamino);
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is trans —CH═CH—, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 5-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-methylaminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compourid of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is. 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyi, r is 1, and R 3 is 4-hydroxy
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 2-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1. is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrimidin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrimidin-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 1, and R 3 is 6-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyrimidin-2-yl, r is 0, and R 3 is absent;
a compound-of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyrimidin-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-2-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 3-pyridin-3-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-2-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 1, and R 3 is 6-methoxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1 H-indol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1 H-indol-6-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-2-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is-(CH 2 ) 2 —, A2 is pyrimidin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 isfphenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is thiophen-2-yl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-carboxy, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 2-hydroxymethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-carboxy, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-aminocarbonyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen-1-yl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-methylcarbonylamino;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is naphthalen- -yl, q is 0, R 2 is absent, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-trifluoromethyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is isoquinolin-5-yl, q is 0, R 2 is absent, A3 is 8-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl,. L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-hydroxymethyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-dimethyl, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 2, R 2 is 3,5-difluoro, A3 is 4-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 0, R 2 is absent, A3 is 6-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyridin-3-yl, q is 1, R 2 is 5-methyl, A3 is 6-pyridin-2-yl, r is 0, and R 3 absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-2-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-methyl, A3 is 4-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 1, R 2 is 3-fluoro, A3 is 4-pyridin-4-yl, r is 0, and R 3 is
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 2-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 3-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 4-hydroxy;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-phenyl, r is 1, and R 3 is 4-hydroxymethyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-3-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is pyrazin-2-yl, q is 0, R 2 is absent, A3 is 5-pyridin-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-2-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-4-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-5-yl, r is 1, and R 3 is 1-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-oxazol-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(4,5-dihydro-oxazol-5-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is ′—-(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-thiazol-4-yl, r is 1, and R 3 is 2-methyl;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-pyrazol-1-yl, r is 2, and R 3 is 3,5-dimethyl
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-thiadiazol-4-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH2) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(1 ,2,4-triazol-1-yl), r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-1H-tetrazol-5-yl, r is 0, and R 3 is absent;
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-imidazol-3-yl, r is 2, and R 3 is 4,5-dichloro; and
a compound of Formula (Ia) wherein R 1 is 4-t-butyl, A1 is phenyl, L is —(CH 2 ) 2 —, A2 is phenyl, q is 0, R 2 is absent, A3 is 4-(2,4-dihydro-pyrazol-2-yl), r is 2, and R 3 is 3-oxo, 5-methyl.
50 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 1 or 2 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
51 . A veterinary composition comprising a compound, salt or solvate according to claim 1 or 2 admixed with a veterinarily acceptable carrier, excipient or diluent.
52 . A method of treating or preventing a disease or condition in a mammal in which the disease or condition is affected by the antagonism of vanilloid type 1 receptors, which method comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 or claim 2 .
53 . A method of treating or preventing a disease or condition in a mammal in which the disease or condition is affected by the agonism of vanilloid type 1 receptors, which method comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 1 or 2 .
54 . The method of claim 52 or 53 wherein the disease or condition is selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, regulation of fever, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, urinary incontinence, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral - peripheral neuropathy, diabetic neuropathy, central pain, neuropathies associated with spinal cord injury, stroke, ALS, Parkinson's disease, or multiple sclerosis, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, menstrual pain, endometriosis, dysmenorrhea, oral neuropathic pain, Charcot's pain, radiculopathy, complex regional pain syndrome I and II (CRPS I/II), Guillain-barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, pain associated with bone cancer, and trauma.
55 . The method of claim 52 or 53 wherein the condition is caused by a disease selected from the group consisting of inflammatory pain, neuropathic pain, visceral pain, pain associated with inflammatory bowel disease, colitis, mechanical hyperalgesia, LPS-induced fever, pyresis, inflammatory bronchial conditions, cough, anxiety, and panic disorders.
56 . The method of claim 53 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 1,000 mg.
57 . The method of claim 53 wherein said therapeutically effective amount comprises a dose range of from about 50 mg to about 1000 mg.
58 . The method of claim 53 wherein said therapeutically effective amount comprises a dose range of from about 100 mg to about 1000 mg.Join the waitlist — get patent alerts
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